Pristinamycin is a mixture of two components that have a synergistic antibacterial action. Pristinamycin IA is a macrolide, and results in pristinamycin's having a similar spectrum of action to erythromycin. Pristinamycin IIA (streptogramin A) is a depsipeptide.[1] PI and PII are coproduced by S. pristinaespiralis in a ratio of 30:70. Each compound binds to the bacterial 50 S ribosomal subunit and inhibits the elongation process of the protein synthesis, thereby exhibiting only a moderate bacteriostatic activity. However, the combination of both substances acts synergistically and leads to a potent bactericidal activity that can reach up to 100 times that of the separate components.

The pristinamycin biosynthetic gene cluster is the largest antibiotic supercluster known so far, with a size of ~210 kb, wherein the PI and PII biosynthetic genes are not clustered individually but are scattered across the complete sequence region.[2] Furthermore, this biosynthetic gene region is interrupted by a cryptic type II PKS gene cluster.

The lack of an intravenous formulation led to the development of the pristinamycin-derivative quinupristin/dalfopristin (i.e., Synercid), which may be administered intravenously for more severe MRSA infections.